Target Information
Target General Infomation | |||||
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Target ID |
T38179
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Former ID |
TTDS00228
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Target Name |
Beta-lactamase
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Gene Name |
blaZ
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Synonyms |
Cephalosporinase; blaZ
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Target Type |
Successful
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Disease | Bacterial infections [ICD9: 001-009, 010-018, 020-027, 030-041, 080-088, 090-099, 100-104; ICD10: A00-B99] | ||||
Gram-positive bacterial infection [ICD9: 001-009, 010-018, 020-027, 030-041, 080-088, 090-099, 100-104] | |||||
Infections [ICD9: 001-139; ICD10: A00-B99] | |||||
Multidrug resistant infection [ICD10: A00-B99] | |||||
Methicillin-resistant staphylococcus aureus infection [ICD10: B95.62] | |||||
Otitis media [ICD10: H65-H67] | |||||
Streptococcus pneumoniae infection [ICD10: J13] | |||||
Serious infections [ICD9: 001-139; ICD10: A00-B99] | |||||
Toxicity [ICD10: T36-T50, T51-T65] | |||||
Unspecified [ICD code not available] | |||||
Function |
This protein is a serine beta-lactamase with a substrate specificity for cephalosporins.
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BioChemical Class |
Carbon-nitrogen hydrolase
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Target Validation |
T38179
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UniProt ID | |||||
EC Number |
EC 3.5.2.6
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Sequence |
MKKLIFLIVIALVLSACNSNSSHAKELNDLEKKYNAHIGVYALDTKSGKEVKFNSDKRFA
YASTSKAINSAILLEQVPYNKLNKKVHINKDDIVAYSPILEKYVGKDITLKALIEASMTY SDNTANNKIIKEIGGIKKVKQRLKELGDKVTNPVRYEIELNYYSPKSKKDTSTPAAFGKT LNKLIANGKLSKENKKFLLDLMLNNKSGDTLIKDGVPKDYKVADKSGQAITYASRNDVAF VYPKGQSEPIVLVIFTNKDNKSDKPNDKLISETAKSVMKEF |
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Drugs and Mode of Action | |||||
Drug(s) | Ceftolozane/tazobactam | Drug Info | Approved | Unspecified | [551871] |
Clavulanate | Drug Info | Approved | Bacterial infections | [538214] | |
Tazobactam | Drug Info | Approved | Bacterial infections | [536361] | |
CAZ AVI | Drug Info | Phase 3 | Serious infections | [523980] | |
CXL | Drug Info | Phase 2 | Methicillin-resistant staphylococcus aureus infection | [550289] | |
MK-7655 | Drug Info | Phase 2 | Bacterial infections | [550004] | |
ME-1071 | Drug Info | Phase 1 | Bacterial infections | [548621] | |
RASV-Sp | Drug Info | Phase 1 | Streptococcus pneumoniae infection | [544359] | |
2085-P | Drug Info | Discontinued in Phase 3 | Otitis media | [544827] | |
DA-7101 | Drug Info | Discontinued in Phase 3 | Gram-positive bacterial infection | [536094] | |
P1A | Drug Info | Discontinued in Phase 2 | Toxicity | [547883] | |
BRL-42715 | Drug Info | Terminated | Bacterial infections | [544791] | |
CL-186659 | Drug Info | Terminated | Bacterial infections | [545772] | |
Ro-48-1220 | Drug Info | Terminated | Bacterial infections | [545783] | |
Ro-48-5545 | Drug Info | Terminated | Bacterial infections | [546440] | |
Ro-48-8724 | Drug Info | Terminated | Multidrug resistant infection | [546449] | |
SB-236049 | Drug Info | Terminated | Bacterial infections | [526339] | |
Inhibitor | (P-Iodophenylacetylamino)Methylphosphinic Acid | Drug Info | [551393] | ||
1-Aminopropane-1,2,3-tricarboxylic acid | Drug Info | [530163] | |||
2-(N-Morpholino)-Ethanesulfonic Acid | Drug Info | [551393] | |||
2-(Sulfanylmethyl)phenylphosphonic acid | Drug Info | [530954] | |||
2-mercaptophenylphosphonic acid | Drug Info | [530954] | |||
2-Methyl-2,4-Pentanediol | Drug Info | [551393] | |||
2-phenyl-1H-imidazole-4-carboxylic acid | Drug Info | [551374] | |||
3-Amino-3-(methoxycarbonyl)-1,5-pentandioic acid | Drug Info | [530163] | |||
3-ethoxycarbonylpyroglutamate | Drug Info | [530163] | |||
3-Nitrophenylboronic Acid | Drug Info | [551393] | |||
4,4'-Biphenyldiboronic Acid | Drug Info | [551393] | |||
4-(Carboxyvin-2-Yl)Phenylboronic Acid | Drug Info | [551393] | |||
4-Carboxyphenylboronic Acid | Drug Info | [551393] | |||
4-iodo-acetamido phenylboronic acid | Drug Info | [551393] | |||
4-Methyl-3-(2-oxo-azetidin-1-yl)-benzoic acid | Drug Info | [533436] | |||
4-[(METHYLSULFONYL)AMINO]BENZOIC ACID | Drug Info | [551374] | |||
5-Fluoro-2-sulfanyl-phenylphosphonic acid | Drug Info | [530954] | |||
5-hydroxymethylbenzo[b]thiophen-2-ylboronic acid | Drug Info | [529114] | |||
5-methyl-benzo[b]thiophen-2-ylboronic acid | Drug Info | [529114] | |||
Acetate Ion | Drug Info | [551393] | |||
Acylated Ceftazidime | Drug Info | [551393] | |||
Alpha-Sulfanyl(2,4-dichlorobenzyl)phosphonic acid | Drug Info | [530954] | |||
Alpha-Sulfanyl(2-methoxybenzyl)phosphonic acid | Drug Info | [530954] | |||
Alpha-Sulfanyl(4-bromobenzyl)phosphonic acid | Drug Info | [530954] | |||
Alpha-Sulfanyl(4-chlorobenzyl)phosphonic acid | Drug Info | [530954] | |||
Alpha-Sulfanyl(4-fluorobenzyl)phosphonic acid | Drug Info | [530954] | |||
Alpha-Sulfanylbenzylphosphonic acid | Drug Info | [530954] | |||
Alpha-Sulfanylpropylphosphonic acid | Drug Info | [530954] | |||
Benzo[b]thiophen-2-ylboronic acid | Drug Info | [529114] | |||
Benzo[B]Thiophene-2-Boronic Acid | Drug Info | [551393] | |||
BRL-42715 | Drug Info | [533347] | |||
Carbamic Acid | Drug Info | [551393] | |||
Clavulanate | Drug Info | [537436] | |||
Clavulanate+Amoxicillin | Drug Info | [536222] | |||
DA-7101 | Drug Info | [536094] | |||
Degraded Cephaloridine | Drug Info | [551393] | |||
Diisopropyl 1-mercaptopropylphosphonate | Drug Info | [530954] | |||
Diisopropyl 2-(sulfanylmethyl)phenylphosphonate | Drug Info | [530954] | |||
Diisopropyl mercapto(phenyl)methylphosphonate | Drug Info | [530954] | |||
Hydrolyzed Cephalothin | Drug Info | [551393] | |||
M-Aminophenylboronic Acid | Drug Info | [551393] | |||
ME-1071 | Drug Info | [532264] | |||
MK-7655 | Drug Info | [532629] | |||
N-2-Thiophen-2-Yl-Acetamide Boronic Acid | Drug Info | [551393] | |||
PCNOTAXIME GROUP | Drug Info | [551374] | |||
Ro-48-5545 | Drug Info | [534491] | |||
SB-236049 | Drug Info | [526339] | |||
Sucrose | Drug Info | [551403] | |||
Tazobactam | Drug Info | [537578] | |||
Thiophene-2-ylboronic acid | Drug Info | [529114] | |||
Tribenzyl 2-aminopropane-1,2,3-tricarboxylate | Drug Info | [530163] | |||
Triethyl 2-aminopropane-1,2,3-tricarboxylate | Drug Info | [530163] | |||
[[N-(Benzyloxycarbonyl)Amino]Methyl]Phosphate | Drug Info | [551393] | |||
Modulator | 2085-P | Drug Info | [550886] | ||
CAZ AVI | Drug Info | [531904] | |||
Ceftolozane/tazobactam | Drug Info | [533123] | |||
CL-186659 | Drug Info | [550886] | |||
CXL | Drug Info | [551120] | |||
P1A | Drug Info | [530289] | |||
Ro-48-1220 | Drug Info | [526280] | |||
Ro-48-8724 | Drug Info | [534754] | |||
References | |||||
Ref 523980 | ClinicalTrials.gov (NCT01644643) Ceftazidime-Avibactam for the Treatment of Infections Due to Ceftazidime Resistant Pathogens. U.S. National Institutes of Health. | ||||
Ref 526339 | Identification of a series of tricyclic natural products as potent broad-spectrum inhibitors of metallo-beta-lactamases. Antimicrob Agents Chemother. 2002 Jun;46(6):1880-6. | ||||
Ref 536094 | Emerging drugs for bacterial urinary tract infections. Expert Opin Emerg Drugs. 2005 May;10(2):275-98. | ||||
Ref 536361 | Natural products as sources of new drugs over the last 25 years. J Nat Prod. 2007 Mar;70(3):461-77. Epub 2007 Feb 20. | ||||
Ref 538214 | FDA Approved Drug Products from FDA Official Website. 2009. Application Number: (ANDA) 065063. | ||||
Ref 544359 | Rapid, Sensitive Recovery of Recombinant Attenuated Salmonella enterica Serovar Typhi Vaccine Strains from Human Blood. Clin Vaccine Immunol. 2013 September; 20(9): 1473-1478. | ||||
Ref 544791 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800001128) | ||||
Ref 544827 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800001248) | ||||
Ref 545772 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800004648) | ||||
Ref 545783 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800004684) | ||||
Ref 546440 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800008139) | ||||
Ref 546449 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800008187) | ||||
Ref 547883 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800020134) | ||||
Ref 526280 | Comparative in vitro activity of apalcillin alone and combined with Ro 48-1220, a novel penam beta-lactamase inhibitor. Clin Microbiol Infect. 1995 Feb;1(2):86-100. | ||||
Ref 526339 | Identification of a series of tricyclic natural products as potent broad-spectrum inhibitors of metallo-beta-lactamases. Antimicrob Agents Chemother. 2002 Jun;46(6):1880-6. | ||||
Ref 529114 | J Med Chem. 2007 Nov 15;50(23):5644-54. Epub 2007 Oct 23.Optimizing cell permeation of an antibiotic resistance inhibitor for improved efficacy. | ||||
Ref 530163 | Bioorg Med Chem Lett. 2009 Jul 1;19(13):3593-7. Epub 2009 May 6.Discovery of novel lipophilic inhibitors of OXA-10 enzyme (class D beta-lactamase) by screening amino analogs and homologs of citrate and isocitrate. | ||||
Ref 530289 | IPSAT P1A, a class A beta-lactamase therapy for the prevention of penicillin-induced disruption to the intestinal microflora. Curr Opin Investig Drugs. 2009 Aug;10(8):838-44. | ||||
Ref 530954 | J Med Chem. 2010 Jul 8;53(13):4862-76.Mercaptophosphonate compounds as broad-spectrum inhibitors of the metallo-beta-lactamases. | ||||
Ref 531904 | NXL104 irreversibly inhibits the beta-lactamase from Mycobacterium tuberculosis. Biochemistry. 2012 Jun 5;51(22):4551-7. Epub 2012 May 22. | ||||
Ref 532264 | Multidrug-resistant Gram-negative bacterial infections: are you ready for the challenge. Curr Clin Pharmacol. 2014 Feb;9(1):27-38. | ||||
Ref 532629 | Discovery of MK-7655, a beta-lactamase inhibitor for combination with Primaxin?. Bioorg Med Chem Lett. 2014 Feb 1;24(3):780-5. | ||||
Ref 533347 | In vitro evaluation of BRL 42715, a novel beta-lactamase inhibitor. Antimicrob Agents Chemother. 1989 Sep;33(9):1580-7. | ||||
Ref 533436 | J Med Chem. 1988 Feb;31(2):370-4.N-aryl 3-halogenated azetidin-2-ones and benzocarbacephems, inhibitors of beta-lactamases. | ||||
Ref 534491 | Potentiation of beta-lactams against Pseudomonas aeruginosa strains by Ro 48-1256, a bridged monobactam inhibitor of AmpC beta-lactamases. J Antimicrob Chemother. 1997 Sep;40(3):335-43. | ||||
Ref 534754 | Activity of a broad-spectrum cephalosporin (Ro 48-8391) alone and in combination with two novel beta-lactamase inhibitors (Ro 48-5545 and Ro 48-8724). Diagn Microbiol Infect Dis. 1998 Oct;32(2):85-94. | ||||
Ref 536094 | Emerging drugs for bacterial urinary tract infections. Expert Opin Emerg Drugs. 2005 May;10(2):275-98. | ||||
Ref 536222 | Emerging therapies for the treatment and prevention of otitis media. Expert Opin Emerg Drugs. 2006 May;11(2):251-64. | ||||
Ref 537436 | A sensitive coupled HPLC/electrospray mass spectrometry assay for SPM-1 metallo-beta-lactamase inhibitors. Assay Drug Dev Technol. 2009 Apr;7(2):170-9. | ||||
Ref 537578 | Selection of TNF-alpha binding affibody molecules using a beta-lactamase protein fragment complementation assay. N Biotechnol. 2009 Jul 1. | ||||
Ref 550148 | WO patent application no. 2010,0456,20, Recombinant bacterium capable of eliciting an immune response against streptococcus pneumoniae. |
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